General Information

General Information

DRAVP ID DRAVPe00573

Peptide Name HR2P-M2

Sequence SLTQINTTLLDLEYEMKKLEEVVKKLEESYIDLKEL

Sequence Length 36

UniProt ID No entry found

Source Synthetic construct

Activity Information

Target Organism MERS-CoV

Assay Inhibition of MERS-CoV S-Protein-Mediated Cell–Cell Fusion Assay

Activity

[Ref.29442512]MERS-CoV:inhibition of cell-cell fusion in Huh-7 cells(EC50=0.75 ± 0.09 μM);
WT MERS-CoV pseudovirus:inhibition of pseudovirus infection in calu-3 cells(EC50=1.07±0.21 μM);
Q1020H-MERS-CoV pseudovirus:inhibition of pseudovirus infection in calu-3 cells(EC50=1.25± 0.18 μM);
Q1020R-MERS-CoV pseudovirus:inhibition of pseudovirus infection in calu-3 cells(EC50=0.64± 0.16 μM).

Hemolytic Activity No hemolysis information or data found in the reference(s) presented in this entry

Cytotoxicity

[Ref.29442512]Calu-3 cell:CC50>100 μM

Binding Target membrane

Mechanism The peptide inhibits MERS-CoV infection and its spike (S) protein-mediated cell–cell fusion.

Structure Information

PDB ID None

Predicted Structure Download DRAVPe00573

Linear/Cyclic Linear

N-terminal Modification Acetylation

C-terminal Modification Amidation

Other Modification None

Stereochemistry L

Physicochemical Information

Formula C193H321N43O64S

Absent amino acids ACFGHPRW

Common amino acids L

Mass 4299.98

Pl 4.48

Basic residues 5

Acidic residues 9

Hydrophobic residues 12

Net charge -4

Boman Index -6020

Hydrophobicity -40.56

Aliphatic Index 124.44

Half Life

Mammalian:1.9 hour
Yeast:>20 hour
E.coli:>10 hour

Extinction Coefficient cystines 2980

Absorbance 280nm 85.14

Polar residues 8

Literature Information

Literature 1

Title Discovery of Hydrocarbon-Stapled Short α-Helical Peptides as Promising Middle East Respiratory Syndrome Coronavirus (MERS-CoV) Fusion Inhibitors.

Pubmed ID 29442512

Reference J Med Chem. 2018 Mar 8;61(5):2018-2026.

Author Wang C, Xia S, Zhang P, Zhang T, Wang W, Tian Y, Meng G, Jiang S, Liu K.

DOI 10.1021/acs.jmedchem.7b01732